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Biomedical subjects

M Gastpar

Publications and source records attributed to M Gastpar.

At least 91 records · Page 5Linked to original sources

Acetylation of maprotiline and desmethylmaprotiline in depressive patients phenotyped with sulfamidine, debrisoquine, and mephenytoin.

A gas chromatographic/mass spectrometric method (using either electron impact or chemical ionisation with methane or ammonia) is described for the quantitative analysis of maprotiline (MP, Ludiomil), N-acetylmaprotiline (AcMP) and N-acetyldesmethylmaprotiline (AcDMP) in whole blood or plasma. In two groups (A and B) of 82 and 53 depressive patients treated clinically with MP for 10 and 21 days, respectively, plasma and whole blood MP was monitored during the treatment. In group A, all subjects were phenotyped with debrisoquine and mephenytoin, and 44 with sulfamidine. 5 patients were poor metabolizers of debrisoquine and 2 of mephenytoin; 18 subjects were fast acetylators of sulfamidine. Traces of AcMP were found only in two patients. AcDMP was present in levels below 2 ng/ml in the plasma of most of the patients in group A. In group B, AcDMP levels between 2.4-14.6 ng/ml of whole blood were found in 9 patients. The mass spectral data suggest the presence of another, unknown MP metabolite interfering partly with the analysis of AcDMP. The presence of AcDMP seemed not to be related to the phenotype of the patients as determined by the pharmacogenetic tests.

Acetylation↗

Epidemiology of depression (Europe and North-America).

The published prevalence rates of depressive disorders have steadily increased during the last 20 years. Despite many methodological and social cultural influences, the increase seems to be real and reasons for this trend are given. Among them, the increase of life expectancy, the urbanization, and the possibility for effective treatment are the most important. Among the interfering variables, symptom changes like actually from depression to anxiety should further be investigated.

Depressive Disorder↗

3H-Imipramine binding sites in platelets of hospitalized psychiatric patients.

The density of platelet 3H-imipramine binding sites has been proposed as a biological marker in psychiatry. We report the range of platelet 3H-imipramine binding in 55 psychiatric patients and 11 control subjects. All blood samples were withdrawn at 2300 h (on the day of hospital admission for patients). With the use of a slight modification of a previously described 3H-imipramine binding method, a mean B max of 1,510 fmole/mg protein (range: 390-5,560; median: 1,450) and a mean Kd of 2.0 nM (range: 0.6-17.0; median: 1.4) were determined for psychiatric patients. For the controls, a mean B max of 1,590 fmole/mg protein (range: 870-2,570; median: 1,440) and a mean Kd of 1.4 nM (range 0.8-2.4; median 1.4) were determined. When patients were subdivided based on ICD-9 psychiatric diagnoses, no significant differences between distinct subgroups of psychiatric patients with respect to B max or Kd values for platelet 3H-imipramine binding could be established. Similarly, no significant difference between psychiatric patients and controls was obtained.

Adolescent↗

Befuraline, its safety and efficacy in depressed inpatients.

Befuraline, a new antidepressant drug, was studied in twenty-nine inpatients with unipolar endogenous depression. The evaluation of patients' condition was made on four different study periods by two assessors using the HDRS, the Beck depression inventory and von Zerssen depression scale. Befuraline, given in oral doses of between 100 and 300 mg/day improved the HDRS total score and the cognitive disturbances to a significant extent (p less than 0.01) after the first week of the treatment. Eleven patients withdrew from the study most of them as a result of intolerance to the stimulatory properties of the drug, however, the response was considered satisfactory in 12 of the 29 patients (41%) mostly in the "retarded depressed" class. As Befuraline proved to be well tolerated, it was continued on an outpatient basis in 11 patients, confirming the absence of clinically important untoward effects.

Aged↗

Studies in general practice: interpractice differences.

Based on results of a recent epidemiological study in general practice, interpractice differences are described and found to be rather marked. They include differences in patients population, case definitions and ability to diagnose nosologic groups. Based on relevant literature and own experiences, measures are described which help to reduce interpractice differences and to improve the quality of study data. Examples of training procedures, exchange of information and technical support are given. As a consequence of the interpractice differences these measures are found to be not only desirable but imperative.

Diagnosis, Differential↗

Efficacy and tolerability of dibenzepin administered by intravenous drip infusion to severely depressed patients.

46 severely depressed inpatients received 10-hour intravenous infusions supplying a dose of 720 mg dibenzepin daily on 2 or some cases 3 successive days. The patients were kept under close psychiatric surveillance and their cardiovascular function was carefully monitored. The shorter infusions were as effective as infusions of the same dose of Noveril over 48 h, and did not lead to a greater frequency or severity of general or cardiovascular side effects. The 10-hour infusion regimen thus represents a new mode of treatment for severe depression which is less demanding both technically and in terms of nursing care.

Administration, Oral↗

[Treatment of therapy-resistant depressions. Results of combined infusion treatment].

230 patients with therapy-resistant depression were given intravenous drip infusion treatment with clomipramine (a predominantly serotonin-uptake inhibitor) and maprotiline (a predominantly noradrenaline-uptake inhibitor), preceded by a five-day tranquilizing regimen with a neuroleptic drug. During the treatment period of 10-20 days the patients were given one infusion daily, while later both antidepressants were taken orally. The neuroleptic drug was given at night from the start of the infusion phase to the end of hospitalization. After four weeks' treatment 68% of the endogenous depressives and 54% of the exhaustion depressives had completely remitted. In patients who fail to respond the infusion regimen can be repeated after carefully rechecking the patient's diagnosis. After discharge and resumption of work the antidepressants should be reduced stepwise. A prerequisite for success in the management of refractory depression is the combination of drug administration with adequate psychotherapeutic and physiotherapeutic measures. The infusion regimen is relatively easy to administer, can be given on an outpatient basis and could be the treatment of choice in the future not only for treatment-resistant depression but also for patients whose depressive state requires rapidly effective antidepressive measures. In view of the encouraging experience obtained to date with this treatment, the World Health Organization is conducting an international collaborative research project involving 12 psychiatric centres to elucidate the effectiveness of intravenous infusion therapy in different races with different dietary habits and varying climatic conditions.

Anthracenes↗

Preliminary studies with citalopram (LU 10-171), a specific 5-HT-reuptake inhibitor, as antidepressant.

1. Ten hospitalized, depressive, female patients above the age of 50 have been treated in a 3 week open trial with citalopram, a specific 5-HT-uptake inhibitor. 2. Six full and two partial responders demonstrate a recovery rate within the well known range for tricyclic antidepressant drugs. 3. Early onset of clinical effect and minimal side effects indicate that citalopram is possible a new effective antidepressant.

Aged↗

Driving ability of depressive patients under antidepressants.

A group of twenty depressive patients was compared during a 3-4 month course of antidepressant therapy (Maprotiline: n = 6, age = 46.1; dibenzepin: n = 4, age = 43.0; lithium: n = 6, age = 44.5; "mixed" (maprotiline, dibenzepin trimeprimine): n = 4, age = 50.2) with a healthy control group (n = 32, age = 38.2) for subjective assessment of their depressive mood and performance as well as objective measurement of variables relating to driving behaviour. The measurements were taken 2-4 weeks after a pre-treatment period (day 1) and after 2-3 months of further therapy (day 2). During therapy, all patients felt "less depressive" and "more capable" in subjective terms. All patient groups made learning progress in the objectively measured variables (psychomotor co-ordination and attentiveness tests). By day 2, the patient groups had almost reached the performance level of the control group, providing they received antidepressant therapy (regardless of the action profile) which was suitable for the basic disorder and the symptoms, and therapy was successful in the opinion of the physician. It may be concluded that depressive patients, assuming suitable antidepressant treatment and good response, are capable of driving while under maintenance therapy.

Adult↗

[Management of treatment-resistant depression without ECT (author's transl)].

Intravenous infusions of clomipramine and maprotiline, preceded by a five-day tranquilising regimen with a neuroleptic drug, were given to 177 patients with treatment-resistant depression. During the treatment period of 10-20 days the patients were given one infusion daily followed by both antidepressants taken orally. The neuroleptic drug was given at night, from the start of the infusion phase to the end of hospitalisation. After four weeks 66% of the endogenous depressions and 53% of the exhaustion depressions had completely regressed. In patients who failed to respond the infusion regimen can be repeated, if necessary with nomifensin (Alival) instead of clomipramine (Anafranil) and maprotiline (Ludiomil) in order to achieve the desired improvement without ECT. In addition to careful diagnosis, a prerequisite for likely success in the management of treatment-resistant depression is the combination of drug administration with adequate psychotherapeutic and physiotherapeutic measures. The infusion regimen is relatively easy to undertake, can also be used on an out-patient basis and could be the treatment of choice in the future, not only for treatment-resistant depressions but also for patients whose depressive state requires rapidly effective antidepressive measures.

Antipsychotic Agents↗